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Elacridar Sale

(Synonyms: 依克立达; GF120918; GW0918; GG918; GW120918) 目录号 : GC17215

An inhibitor of MRP-1 and BCRP

Elacridar Chemical Structure

Cas No.:143664-11-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥546.00
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10mg
¥452.00
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50mg
¥1,638.00
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100mg
¥2,195.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment [1]:

Cell lines

Human renal carcinoma cell lines 786-O and human breast cancer cell line MCF-7

Preparation method

The solubility of this compound in DMSO is > 56.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

5 μM, 24 h

Applications

Elacridar is a P-glycoprotein inhibitor that also block ABC Sub-family B Member 2 (ABCG2). Elacridar significantly enhanced sunitinib-induced cytotoxicity in 786-O cells. Confirmed by P-glycoprotein function assay, P-glycoprotein activity was inhibited by elacridar.

Animal experiment [2]:

Animal models

10-14-week wild-type, Abcb1a/1b-/-, 32Abcg2-/-27 and Abcb1a/1b/Abcg2-/- mice, all of a >99% FVB genetic background

Dosage form

Oral administration, 100 mg/kg

Application

Elacridar significantly increased sunitinib brain accumulation in wild-type mice (12-fold), to levels equal to those in Abcb1a/1b/Abcg2-/- mice. The sunitinib brain concentrations were not significantly affected by elacridar treatment in Abcb1a/1b/Abcg2-/- mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Sato H, Siddig S, Uzu M, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells[J]. European journal of pharmacology, 2015, 746: 258-266.

[2]. Tang S C, Lagas J S, Lankheet N A G, et al. Brain accumulation of sunitinib is restricted by P‐glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration[J]. International journal of cancer, 2012, 130(1): 223-233.

产品描述

Elacridar is a potent inhibitor of P-glycoprotein with IC50 values of 193 nM. [1]

P-glycoprotein (permeability glycoprotein) is an important membrane protein. It pumps many foreign substances out of cells. P-glycoprotein belongs to the MDR/TAP subfamily. P-glycoprotein is transmembrane glycoprotein which is about 170 kDa. It is expressed in certain cell types primarily in the pancreas, liver, colon and kidney. It contains 6 transmembrane domains in the N-terminal half of the molecule. It also contains an ATP-binding site in the large cytoplasmic domain. P-glycoprotein binds to the substrate at the cytoplasmic side of the protein. When ATP binds to the cytoplasmic side, the substrate was excreted from the cell. P-glycoprotein can pump toxins or drugs back into the intestinal lumen, pumps them into bile ducts in liver cells.In some cancer cells, P-glycoprotein is overexpressed. It is involved in multidrug resistance of cancer cells.[2]

Elacridar can significantly inhibit the activity of P-glycoprotein at 1μM in MDCKII cells which overexpress P-glycoprotein.[3] In the parental MDCK-II cells, elacridar at 5μM completely inhibit the polarized sunitinib transport.[4] Elacridar did not inhibit the activity of several human cytochromeP450 enzymes in vitro. The absolute bioavailability was about 0.47 and 1.3 respectively, when elacridar was given in the orally and microemulsion, intraperitoneally at 10 mg/kg in mice.[3] Elacridar also can significantly increase sunitinib brain accumulation levels in mice at 10 mg/kg.[4]

References:
[1].  Bankstahl JP, Bankstahl M, Romermann K, Wanek T, Stanek J, Windhorst AD, Fedrowitz M, Erker T, Muller M, Loscher W et al: Tariquidar and elacridar are dose-dependently transported by P-glycoprotein and Bcrp at the blood-brain barrier: a small-animal positron emission tomography and in vitro study. Drug Metab Dispos, 41(4):754-762.
[2].  Aller SG, Yu J, Ward A, Weng Y, Chittaboina S, Zhuo R, Harrell PM, Trinh YT, Zhang Q, Urbatsch IL et al: Structure of P-glycoprotein reveals a molecular basis for poly-specific drug binding. Science 2009, 323(5922):1718-1722.
[3].  Sane R, Mittapalli RK, Elmquist WF: Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability. J Pharm Sci, 102(4):1343-1354.
[4].  Tang SC, Lagas JS, Lankheet NA, Poller B, Hillebrand MJ, Rosing H, Beijnen JH, Schinkel AH: Brain accumulation of sunitinib is restricted by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) and can be enhanced by oral elacridar and sunitinib coadministration. Int J Cancer, 130(1):223-233.

Chemical Properties

Cas No. 143664-11-3 SDF
别名 依克立达; GF120918; GW0918; GG918; GW120918
化学名 N-[4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)ethyl]phenyl]-5-methoxy-9-oxo-10H-acridine-4-carboxamide
Canonical SMILES COC1=CC=CC2=C1NC3=C(C2=O)C=CC=C3C(=O)NC4=CC=C(C=C4)CCN5CCC6=CC(=C(C=C6C5)OC)OC
分子式 C34H33N3O5 分子量 563.64
溶解度 ≥ 56.4 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7742 mL 8.8709 mL 17.7418 mL
5 mM 0.3548 mL 1.7742 mL 3.5484 mL
10 mM 0.1774 mL 0.8871 mL 1.7742 mL
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